Compositions of tiacumicins stabilized with antioxidants

摘要

Disclosed is a pharmaceutical composition to treat or prevent C. difficile infection in a subject, comprising a therapeutically effective amount of one or more tiacumicins, a stabilizing amount of one or more antioxidants, and one or more pharmaceutically acceptable excipients, wherein one or more tiacumicins is Difimicin, also described as 3-[[[6-Deoxy-4-O-(3,5-dichloro-2-ethyl-4,6-dihydroxybenzoyl)-2-O-methyl-D-mannopyranosyl]oxy]-methyl]-12(R)-[[6-deoxy-5-C-15 methyl-4-O-(2-methyl-1-oxopropyl)-D-lyxohexopyranosyl] oxy]-11(S)-ethyl-8(S)-hydroxy-18(S)-(1(R)hydroxyethyl)-9,13,15-trimethyloxacyclooctadeca- 3,5,9,13,15-pentaene-2-one the composition is in a solid dosage form wherein the infection is C. difficile-associated diarrhea (CDAD), colitis, pseudomembranous colitis, antibiotic associated diarrhea antibiotic-associated enterocolitis, sporadic enterocolitis, nosocomial enterocolitis, colitis membranous, infectious diarrhea, and irritable bowel syndrome.